Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 10, Issue 4, Pages 499-503Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.8b00532
Keywords
cancer; NHERFI; PDZ domain; beta-catenin; drug design; synthesis
Categories
Funding
- Italian PRIN 2015 [2015FCHJ8E]
- Sapienza University [RP11715C7D1CF0D1]
- AIRC-IG [14236, 17575]
- AFM-Telethon [21025]
- Institute Pasteur Italy
- European Union [675341]
- Marie Curie Actions (MSCA) [675341] Funding Source: Marie Curie Actions (MSCA)
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Targeted approaches aiming at modulating NHERFI activity, rather than its overall expression, would be preferred to preserve the normal functions of this versatile protein. We focused our attention on the NHERF1/PDZ1 domain that governs its membrane recruitment/displacement through a transient phosphorylation switch. We herein report the design and synthesis of novel NHERF1 PDZ1 domain inhibitors. These compounds have potential therapeutic value when used in combination with antagonists of beta-catenin to augment apoptotic death of colorectal cancer cells refractory to currently available Wnt/beta-catenin-targeted agents.
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